Cariprazine: chemistry, pharmacodynamics, pharmacokinetics, and metabolism, clinical efficacy, safety, and tolerability

@article{Citrome2013CariprazineCP,
  title={Cariprazine: chemistry, pharmacodynamics, pharmacokinetics, and metabolism, clinical efficacy, safety, and tolerability},
  author={Leslie Citrome},
  journal={Expert Opinion on Drug Metabolism \& Toxicology},
  year={2013},
  volume={9},
  pages={193 - 206}
}
  • L. Citrome
  • Published 15 January 2013
  • Medicine, Psychology
  • Expert Opinion on Drug Metabolism & Toxicology
Introduction: Cariprazine is an atypical antipsychotic in clinical development for the treatment of schizophrenia and bipolar mania/mixed episodes. Areas covered: The purpose of this review is to describe the chemistry, pharmacodynamic profile, pharmacokinetics, and clinical profile of cariprazine. Expert opinion: Cariprazine is a dopamine D3-preferring D3/D2 receptor partial agonist. Doses ≥ 1.5 mg/d yielded 69 – 75% D2/D3 receptor occupancy as measured in positron emission tomography scans… 
A new generation of antipsychotics: pharmacology and clinical utility of cariprazine in schizophrenia
TLDR
Well-designed clinical trials, mainly direct “head-to-head” comparisons with other second-generation antipsychotic agents, are needed to define the therapeutic role and safety profile of cariprazine in schizophrenia and bipolar mania.
Population Pharmacokinetics of Cariprazine and its Major Metabolites
TLDR
Populations pharmacokinetic modeling provided a quantitative description of the concentration-time profile of cariprazine and its metabolites, and a post hoc analysis found that CYP2D6 metabolizer status was not associated with changes in exposure levels for carIPrazine, DCAR, or DDCAR.
Cariprazine for the Treatment of Schizophrenia: A Review of this Dopamine D3-Preferring D3/D2 Receptor Partial Agonist.
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  • Psychology, Medicine
    Clinical schizophrenia & related psychoses
  • 2016
TLDR
Cariprazine is an antipsychotic medication and received approval by the U.S. Food and Drug Administration for the treatment of schizophrenia in September 2015; the starting dose of 1.5 mg/d is potentially therapeutic.
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TLDR
Once-daily cariprazine was generally well tolerated in adult patients with schizophrenia, and exposure was dose proportional over the range of 3–9 mg/day.
Preclinical pharmacodynamic and pharmacokinetic characterization of the major metabolites of cariprazine
TLDR
Overall, in vitro and in vivo pharmacological profiles of DCAR and DDCAR demonstrated high similarity with cariprazine, suggesting that the major metabolites of carIPrazine contribute significantly to its clinical efficacy.
The preclinical discovery and development of cariprazine for the treatment of schizophrenia
TLDR
This review article focuses on the preclinical discovery of cariprazine providing details regarding its pharmacological, behavioral, and neurochemical mechanisms and its contribution to clinical therapeutic benefits.
Cariprazine for acute and maintenance treatment of adults with schizophrenia: an evidence-based review and place in therapy
  • L. Citrome
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    Neuropsychiatric disease and treatment
  • 2018
TLDR
For the approved dose range, rates of discontinuation because of an adverse event were lower overall for patients receiving cariprazine vs placebo, and weight and metabolic profile appear favorable.
Clinical Pharmacokinetics of Atypical Antipsychotics: An Update
TLDR
Optimal plasma concentration ranges are proposed for clozapine, risperidone, paliperidone and olanzapine because the studies of quetiapine and amisulpride provide only limited information and there is no direct evidence concerning ziprasid one, aripiprazole, sertindole, brexpiprazoles and cariprazine.
Cariprazine - a novel antipsychotic drug and its place in the treatment of schizophrenia.
TLDR
Overall, current evidence in the field supports the use of cariprazine in exacerbation of schizophrenia and suggests promising efficacy in the treatment of predominant negative symptoms.
Negative Symptoms of Schizophrenia: New Prospects of Cariprazine Treatment
TLDR
There is evidence to suggest cariprazine is effective in treatment-resistant cases, but this requires further confirmation, and further studies are needed to collect more data on long-term treatment of schizophrenia and especially negative symptoms.
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